Cysmethynil

Cysmethynil

CAT N°: 14745
Price:

From 122.00 103.70

Post-translational protein prenylation is a 3-step process that occurs at the C-terminus of a number of proteins involved in cell growth control and oncogenesis. Isoprenylcysteine carboxyl methyltransferase (Icmt) catalyzes the methylation of C-terminal prenylcysteine residues, the last step in this process. Cysmethynil is an indole-based, time-dependent inhibitor of Icmt (IC50 = i = 0.14 µM for the final complex).{23512} It does not inhibit other enzymes in the prenylation pathway (farensyltransferase, geranylgeranyltransferase type I, and Rce1) at concentrations up to 50 µM, or related methyltransferases.{23511} Treatment of cancer cells results in a dose-dependent decrease in Ras carboxylmethylation, mislocalization of Ras, and impaired signaling through Ras pathways.{23511} Treatment of PC3 prostate cancer cells with 25 µM cysmethynil resulted in decreased mTOR signaling, accumulation of cells in the G1 phase, and autophagy-mediated cell death.{23510}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 5-(3-methylphenyl)-1-octyl-1H-indole-3-acetamide
  • Correlated keywords
    • isoprenylcysteines carboxyl methyltransferases Icmts prenylation inhibitors inhibits inhibitions autophagy cancers post-translational modifications cells signaling methylation signals modify indole-based indoles based time-dependent times dependent substrates S-adenosylmethionine adenosylmethionine treatments Ras carboxylmethylation pathways PC3 prostates G1 phases G-1 Gs 1 one autophagy-mediated autophagy mediated deaths proteins protein lipidation
  • Product Overview:
    Post-translational protein prenylation is a 3-step process that occurs at the C-terminus of a number of proteins involved in cell growth control and oncogenesis. Isoprenylcysteine carboxyl methyltransferase (Icmt) catalyzes the methylation of C-terminal prenylcysteine residues, the last step in this process. Cysmethynil is an indole-based, time-dependent inhibitor of Icmt (IC50 = i = 0.14 µM for the final complex).{23512} It does not inhibit other enzymes in the prenylation pathway (farensyltransferase, geranylgeranyltransferase type I, and Rce1) at concentrations up to 50 µM, or related methyltransferases.{23511} Treatment of cancer cells results in a dose-dependent decrease in Ras carboxylmethylation, mislocalization of Ras, and impaired signaling through Ras pathways.{23511} Treatment of PC3 prostate cancer cells with 25 µM cysmethynil resulted in decreased mTOR signaling, accumulation of cells in the G1 phase, and autophagy-mediated cell death.{23510}

We also advise you